Quinazolines as cyclin dependent kinase inhibitors

被引:87
作者
Sielecki, TM [1 ]
Johnson, TL
Liu, J
Muckelbauer, JK
Grafstrom, RH
Cox, S
Boylan, J
Burton, CR
Chen, HY
Smallwood, A
Chang, CH
Boisclair, M
Benfield, PA
Trainor, GL
Seitz, SP
机构
[1] DuPont Pharmaceut Co, Wilmington, DE 19880 USA
[2] Mitotix Inc, Cambridge, MA 02139 USA
关键词
D O I
10.1016/S0960-894X(01)00185-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Quinazolines have been identified as inhibitors of CDK4/D1 and CDK2/E. Aspects of the SAR were investigated using solution-phase. parallel synthesis. An X-ray crystal structure was obtained of quinazoline 51 bound in CDK2 and key interactions within the ATP binding pocket are defined. (C) 2001 DuPont Pharmaceuticals Company. Published by Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1157 / 1160
页数:4
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